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In both animals and humanscabergoline is extensively metabolizedpredominately via hydrolysis of the acylurea bond or the urea moietyCytochrome P-450 mediated metabolism appears to be minimalCabergoline does not cause enzyme induction and/or inhibition in the ratHydrolysis of the acylurea or urea moiety abolishes the prolactin-lowering effect of cabergolineand major metabolites identified thus far do not contribute to the therapeutic effect.

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Following single oral doses of 0.5 mg to 1.5 mg given to 12 healthy adult volunteersmean peak plasma levels of 30 to 70 picogramspgmL of cabergoline were observed within 2 to 3 hoursOver the 0.5-to-7 mg dose rangecabergoline plasma levels appeared to be doseproportional in 12 healthy adult volunteers and nine adult parkinsonian patientsA repeat-dose study in 12 healthy volunteers suggests that steady-state levels following a once-weekly dosing schedule are expected to be twofold to threefold higher than after a single doseThe absolute bioavailability of cabergoline is unknownA significant fraction of the administered dose undergoes a first-pass effectThe elimination half-life of cabergoline estimated from urinary data of 12 healthy subjects ranged between 63 to 69 hoursThe prolonged prolactin-lowering effect of cabergoline may be related to its slow elimination and long half-life.

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